Research article summary (published 29 Aug 2009):

Membrane cholesterol depletion from live cells enhances the function of human serotonin(1A) receptors.

Full Abstract

Work from our laboratory has previously demonstrated the requirement of membrane cholesterol in the function of the serotonin(1A) receptor, a member of the G-protein coupled receptor (GPCR) superfamily. In order to monitor the effect of cellular organization on the function of human serotonin(1A) receptors, we explored receptor function following cholesterol depletion in live cells and membranes isolated from cholesterol-depleted cells. We report here the novel observation that while ligand binding of serotonin(1A) receptors displays an increase in membranes isolated from cholesterol-depleted cells, such trend is absent when binding is performed on cholesterol-depleted intact cells. Importantly, we show here, for the first time, that G-protein coupling of the serotonin(1A) receptor is enhanced in membranes isolated from cholesterol-depleted cells. These results assume pharmacological relevance in view of the recently described structural evidence of specific cholesterol binding sites in GPCRs, and may help in designing better therapeutic strategies for diseases related to GPCRs.

Author information

Author/s: Prasad, Rajesh (R); Paila, Yamuna Devi (YD); Jafurulla, Md (M); Chattopadhyay, Amitabha (A);

Affiliation: Centre for Cellular and Molecular Biology, Council of Scientific and Industrial Research, Uppal Road, Hyderabad 500 007, India.

Journal and publication information

Publication Type: Journal Article; Research Support, Non-U.S. Gov't

Journal: Biochemical and biophysical research communications (Biochem Biophys Res Commun), published in United States. (Language: eng)

Reference: 2009-Nov; vol 389 (issue 2) : pp 333-7

Dates: Created 2009/09/29; Completed 2009/10/14;

PMID: 19723504, status: MEDLINE (last retrieval date: 10/14/2009, IMS Date: )

Sourced from the National Library of Medicine. Abstract text and other information may be subject to copyright.

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MeSH headings (categories)

This article was linked to the MESH Headings shown below.

Animals CHO Cells Cell Membrane - metabolism Cholesterol - metabolism Cricetinae

Cricetinae Cricetulus Humans Ligands Receptor, Serotonin, 5-HT1A - genetics; metabolism

Associated Chemicals: Ligands (0) ; Receptor, Serotonin, 5-HT1A (112692-38-3) ; Cholesterol (57-88-5)

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